Abstract：
:The oral dose metabolism of dilazep dihydrochloride [tetrahydro-1H-1,4-diazepine-1,4(5H)-dipropanol 3,4,5-trimethoxybenzoate] was examined in six hypertensive patients receiving a single oral dose of 600 mg of dilazep (3-3.8 mg/kg BW). Blood was collected at 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, and 24 h after administration of the dose and urine was collected for three time intervals of 0-4 h, 4-10 h, and 10-24 h. Dilazep concentrations in blood and urine were determined by high-performance liquid chromatography. Dilazep decayed monoexponentially with a mean elimination rate constant of 0.27 +/- 0.13 h-1 and a mean half-life of 3.04 +/- 1.34 h. The mean tmax of absorption was 1.40 +/- 0.82 h. With maximally tolerated chronic doses, the steady-state concentration measured at 1 week was 25.6 ng/mL in a patient receiving 300 mg daily (100 mg TID) for 3 weeks, and dilazep concentration increased with the dose in others for up to a 600-mg dose daily. Dilazep did not produce any significant changes in heart rate and blood pressure after a single oral dose or during chronic dosing. There was no correlation between blood dilazep levels and the changes in heart rate and blood pressure. In three additional patients, oral dilazep dihydrochloride titrated gradually to maximally tolerated doses (900 mg daily) failed to produce significant effects on biochemical and neurohumoral measurements, and hemodynamic parameters as well as ventricular functional indices measured by radionucleide methods. Oral dilazep administration in maximally tolerated doses is devoid of effects on blood pressure and cardiac hemodynamic function.
journal_name
J Pharm Scijournal_title
Journal of pharmaceutical sciencesauthors
Sambhi MP,Kannan R,Thananopavarn C,Ookhtens M,Gudenzi Mdoi
10.1002/jps.2600780404subject
Has Abstractpub_date
1989-04-01 00:00:00pages
281-4issue
4eissn
0022-3549issn
1520-6017pii
S0022-3549(15)47943-2journal_volume
78pub_type
杂志文章abstract：:It has been shown that significant pore induction (electroporation) occurs in human epidermal membrane (HEM) during iontophoresis even at moderate applied voltages (1-10 V). Recent efforts in our laboratory have been aimed at quantifying HEM electroporation by examining the proportionality between flux enhancement due...
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abstract：:The antimalarial endoperoxides, such as artemisinin, are postulated to exert their potent parasiticidal activity via the formation of reactive intermediates in the iron-rich infected erythrocyte. The in vitro chemical reaction profile of putative endoperoxide antimalarials and ferrous iron is often qualitatively used ...
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doi：10.1016/j.xphs.2019.10.017
更新日期：2020-01-01 00:00:00
abstract：:In this study, we developed cationic microemulsions containing a protein transduction domain (penetratin) for optimizing paclitaxel localization within the skin. Microemulsions were prepared by mixing a surfactant blend (BRIJ:ethanol:propylene glycol 2:1:1, w/w/w) with monocaprylin (oil phase) at 1.3:1 ratio, and addi...
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pub_type： 杂志文章
doi：10.1002/jps.23482
更新日期：2013-05-01 00:00:00
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doi：10.1002/jps.2600661023
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journal_title：Journal of pharmaceutical sciences
pub_type： 杂志文章
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journal_title：Journal of pharmaceutical sciences
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doi：10.1002/jps.2600720919
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journal_title：Journal of pharmaceutical sciences
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journal_title：Journal of pharmaceutical sciences
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journal_title：Journal of pharmaceutical sciences
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journal_title：Journal of pharmaceutical sciences
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doi：10.1002/jps.2600730234
更新日期：1984-02-01 00:00:00
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更新日期：1999-11-01 00:00:00
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journal_title：Journal of pharmaceutical sciences
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doi：10.1002/jps.2600680438
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journal_title：Journal of pharmaceutical sciences
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pub_type： 临床试验,杂志文章,随机对照试验
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journal_title：Journal of pharmaceutical sciences
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journal_title：Journal of pharmaceutical sciences
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journal_title：Journal of pharmaceutical sciences
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journal_title：Journal of pharmaceutical sciences
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